- HETEROCYCLIC COMPOUNDS
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The present invention relates to compounds of the general formula (1) wherein the variables are defined as given in the description and claims. The invention further relates to uses of and to, processes and intermediates related to compounds of the general formula (I), wherein Q is wherein the substituents of I, Ia and Ib are as defined in description and claims.
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Paragraph 83
(2018/07/29)
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- PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES
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Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
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Page/Page column 63
(2012/10/07)
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- PYRROLOPYRIDAZINE JAK3 INHIBITORS AND THEIR USE FOR THE TREATMENT OF INFLAMMATORY AND AUTOIMMUNE DISEASES
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Disclosed are compounds of Formula (I), and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.
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Page/Page column 73; 74
(2012/10/07)
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- HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
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Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
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Page/Page column 24
(2011/08/06)
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- 1,1′-Bipyrroles: Synthesis and stereochemistry
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(Chemical Equation Presented) 1,1′-Bipyrrole is synthesized in four steps from hydrazine. A colorless solid, mp 52°C, it sublimes readily at room temperature and forms X-ray quality crystals in which the rings are not coplanar but are nearly orthogonal.
- Dey, Sanjeev K.,Lightner, David A.
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p. 9395 - 9397
(2008/03/13)
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- Electrophotographic organophotoreceptors with novel charge transport compounds
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A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes: (a) a novel charge transport compound having the formula ?where R1 and R2 are selected so that R1 and R
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- Compounds specific to adenosine A1 receptors and uses thereof
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This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
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- Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
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Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
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- Compounds specific to adenosine A1 receptors and uses thereof
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This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.
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- Tautomerism in the solid state and in solution of a series of 6-aminofulvene-1-aldimines
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To study systems able to sustain intramolecular proton-transfer, we have prepared a series of six aminofulvene aldimines including several labeled with 15N and 2H. These compounds show coupling constants through the hydrogen bond, 1hJ(15N-1H) and 2hJ(15N-15N). The position of the tautomeric equilibria, i.e., on what nitrogen atom is the proton, was determined in the solid state and in solution. The crystal structure of N{([5-[(phenylamino)methylene]- 1,3-cyclopentadien-1-yl]methylene})pyrrole-1-amine (3) has been determined by X-ray analysis. In solution, both N-H and C-H tautomers were observed and their structures assigned by NMR spectroscopy. Particularly useful is the value of the 1J(15N-1H) coupling constant.
- Sanz, Dionisia,Perez-Torralba, Marta,Alarcon, Sergio Hugo,Claramunt, Rosa Maria,Foces-Foces, Concepcion,Elguero, Jose
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p. 1462 - 1471
(2007/10/03)
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- N-(substituted amino)pyrrole derivatives, and herbicidal compositions
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This invention is to provide an N-(substituted amino)pyrrole derivative represented by the formula (I): which is used as an effective ingredient of herbicidal compositions: STR1 wherein R2, R3, R4 and R5 is independently hydrogen atom, halogen atom, C1 -C4 alkyl group, (C1 -C4 alkyl)carbonyl group, (C3 -C6 cycloalkyl) carbonyl group, (C1 -C4 haloalkyl)carbonyl group, (C3 -C5 alkenyl)carbonyl group, benzoyl group which may be substituted with 1-3 halogen atoms and/or C1 -C4 alkyl groups, N,N-[(di-C1 -C4 alkyl)amino]carbonyl group, (C1 -C4 alkoxy)carbonyl group, etc., X1 and X2 are independently hydrogen atom, halogen atom, C1 -C4 alkyl group, C1 -C4 alkoxy group, etc., and Z is nitrogen atom or CH.
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- Studies on the Synthesis of Phytochrome and Related Tetrapyrroles. Dihydropyrromethenones by Photochemical Rearrangement of N-Pyrrolo Enamides
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Dihydropyrromethenone 67b, a potential precursor for the synthesis of phytochrome 1, has been prepared in enantiomerically pure form beginning with N-aminopyrrole 64 and the acetylenic acid 62b. The key step involved a 3,5-sigmatropic rearrangement of N-pyrrolo enamide 66b.
- Jacobi, Peter A.,Buddhu, Subhas C.,Fry, Douglas,Rajeswari
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p. 2894 - 2906
(2007/10/03)
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- Substituted (pyrroloamino)pyridines: potential agents for the treatment of Alzheimer's disease.
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A novel series of substituted (pyrroloamino)pyridines was synthesized, and the compounds were evaluated for cholinomimetic-like properties in vitro (inhibition of [3H]quinuclidinyl benzilate binding) and in vivo (reversal of scopolamine-induced dementia)
- Davis, Larry,Olsen, Gordon E.,Klein, Joseph T.,Kapples, Kevin J.,Huger, Francis P.,et al.
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p. 582 - 587
(2007/10/03)
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- 3-substituted cephem compounds
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The present invention relates to novel cephalosporins of the formula (I); STR1 wherein, R1 represents a C1 ?C4 alkyl group or STR2 wherein, R2 and R3, independently, represent hydrogen or a C1 ?C3 alkyl group and R4 represents hydrogen or a C1 ?C4 alkyl group; R1a represents hydrogen or an amino-protecting group; Q represents CH or N; and the formula STR3 represents a saturated or unsaturated heterocyclic group which contains 1 to 4 nitrogen atoms of which one is substituted with an amino group to form quaternary ammonium, and oxygen or sulfur, or a fused heterocyclic group thereof formed together with a substituted or unsubstituted benzene or an optional heterocyclic group, or a pharmaceutically acceptable salt thereof, to processes for preparing the same and to a pharmaceutical composition containing the same as an active ingredient. The compounds(1) according to the invention exhibit potent antibacterial activity and broad antibacterial spectrum against the Gram-positive strains including Staphylococcus as well as Gram-negative strains including Pseudomonas, and, therefore, are expected to be very useful in treatment of various diseases caused by bacterial infection in human beings and animals.
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- A NOVEL SYNTHESIS OF PYRROMETHENONES
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Pyrromethenones are prepared by a process involving acylation of an N-aminopyrrole with a suitable acetylenic acid, followed by sequential 5-exo-dig cyclization and 3,5-sigmatropic shift.
- Jacobi, Peter A.,Buddhu, Subhas C.
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p. 4823 - 4826
(2007/10/02)
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